Cayman MGCD-265

MGCD-265 is an inhibitor of c-Met and VEGFR2 (IC₅₀s = 0.029 and 0.01 µM, respectively). It is selective for c-Met and VEGFR2 over Chk1, EGFR, GSK3β, IGF-1R, IKKβ, JAK2, and JNK1 at 0.1 µM but also inhibits VEGFR1, VEGFR3, Ron, Tie2, FLT3, c-Kit, Abl, and TrkA with percent inhibition values ranging from 80 to 100% at 0.1 µM. MGCD-265 also binds to Smoothened (Smo) in HEK293T cell membranes expressing the human receptor (K_i = 0.0417 µM for the wild-type receptor) and inhibits Gli1-mediated transcription in a reporter assay in gefitinib-resistant HCC827 non-small cell lung cancer (NSCLC) cells. It inhibits migration of A549 NSCLC cells induced by hepatocyte growth factor (HGF) and VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC₅₀s = 2 and 0.025 µM, respectively). MGCD-265 (20 mg/kg) reduces tumor growth in several mouse xenograft models, including prostate, colorectal, and gastric cancer models.

WARNING This product is not for human or veterinary use.